The role interplay between mesoporous silica pore volume and surface area and their effect on drug loading capacity

In this study, the influence of the mesoporous silica (MS) textural properties (surface area, pore diameter, and pore volume) on drug loading capacity (monomolecular loading capacity and pore filling capacity) was investigated theoretically and experimentally using a thermoanalytical method. The loa...

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Main Authors: Christoffer G. Bavnhøj, Matthias M. Knopp, Cecilie M. Madsen, Korbinian Löbmann
Format: Article
Language:English
Published: Elsevier 2019-12-01
Series:International Journal of Pharmaceutics: X
Online Access:http://www.sciencedirect.com/science/article/pii/S2590156719300222
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author Christoffer G. Bavnhøj
Matthias M. Knopp
Cecilie M. Madsen
Korbinian Löbmann
author_facet Christoffer G. Bavnhøj
Matthias M. Knopp
Cecilie M. Madsen
Korbinian Löbmann
author_sort Christoffer G. Bavnhøj
collection DOAJ
description In this study, the influence of the mesoporous silica (MS) textural properties (surface area, pore diameter, and pore volume) on drug loading capacity (monomolecular loading capacity and pore filling capacity) was investigated theoretically and experimentally using a thermoanalytical method. The loading capacities of three model drugs (celecoxib, cinnarizine, and paracetamol) were determined in five different MS grades of Sylysia® with identical chemical composition, but varying surface area, pore diameter and pore volume. The experimentally determined loading capacities were compared to theoretical loading capacities, calculated based on the surface area and amorphous density of the drugs, and the surface area and pore volume of the MS. The findings of the study showed that the monomolecular loading capacity generally increased with increasing surface area and decreasing pore volume of the MS. However, the MS grade with the highest surface area did not display the highest monomolecular loading capacity for any of the three drugs. This was probably a result of the decreasing pore diameter necessary to accommodate the increasing surface area of the MS i.e., if the pore is smaller than the drug molecule, the drug cannot access the available surface area. For these systems, the amorphous density of the drug and the pore volume of the MS was used to estimate the theoretical pore filling capacity, which was in good agreement with the experimentally determined loading capacity. In conclusion, this study showed that both the pore volume and surface area of the MS will have an influence on the drug loading capacity and that this can be estimated with good accuracy both theoretically and experimentally. Keywords: Mesoporous silica, Loading capacity, Differential scanning calorimetry (DSC), Poorly soluble drugs, Amorphous stability, Surface area, Pore volume, Pore diameter
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spelling doaj.art-66fbedaae20a4ac4ad28ffc6da5087762022-12-22T01:30:37ZengElsevierInternational Journal of Pharmaceutics: X2590-15672019-12-011The role interplay between mesoporous silica pore volume and surface area and their effect on drug loading capacityChristoffer G. Bavnhøj0Matthias M. Knopp1Cecilie M. Madsen2Korbinian Löbmann3Department of Pharmacy, University of Copenhagen, DK-2100 Copenhagen, DenmarkBioneer: FARMA, Department of Pharmacy, DK-2100 Copenhagen, Denmark; Corresponding author at: Bioneer: FARMA, Department of Pharmacy, Universitetsparken 2, DK-2100 Copenhagen, Denmark.Pharmaceutical R&D, H. Lundbeck A/S, DK-2500 Valby, DenmarkDepartment of Pharmacy, University of Copenhagen, DK-2100 Copenhagen, DenmarkIn this study, the influence of the mesoporous silica (MS) textural properties (surface area, pore diameter, and pore volume) on drug loading capacity (monomolecular loading capacity and pore filling capacity) was investigated theoretically and experimentally using a thermoanalytical method. The loading capacities of three model drugs (celecoxib, cinnarizine, and paracetamol) were determined in five different MS grades of Sylysia® with identical chemical composition, but varying surface area, pore diameter and pore volume. The experimentally determined loading capacities were compared to theoretical loading capacities, calculated based on the surface area and amorphous density of the drugs, and the surface area and pore volume of the MS. The findings of the study showed that the monomolecular loading capacity generally increased with increasing surface area and decreasing pore volume of the MS. However, the MS grade with the highest surface area did not display the highest monomolecular loading capacity for any of the three drugs. This was probably a result of the decreasing pore diameter necessary to accommodate the increasing surface area of the MS i.e., if the pore is smaller than the drug molecule, the drug cannot access the available surface area. For these systems, the amorphous density of the drug and the pore volume of the MS was used to estimate the theoretical pore filling capacity, which was in good agreement with the experimentally determined loading capacity. In conclusion, this study showed that both the pore volume and surface area of the MS will have an influence on the drug loading capacity and that this can be estimated with good accuracy both theoretically and experimentally. Keywords: Mesoporous silica, Loading capacity, Differential scanning calorimetry (DSC), Poorly soluble drugs, Amorphous stability, Surface area, Pore volume, Pore diameterhttp://www.sciencedirect.com/science/article/pii/S2590156719300222
spellingShingle Christoffer G. Bavnhøj
Matthias M. Knopp
Cecilie M. Madsen
Korbinian Löbmann
The role interplay between mesoporous silica pore volume and surface area and their effect on drug loading capacity
International Journal of Pharmaceutics: X
title The role interplay between mesoporous silica pore volume and surface area and their effect on drug loading capacity
title_full The role interplay between mesoporous silica pore volume and surface area and their effect on drug loading capacity
title_fullStr The role interplay between mesoporous silica pore volume and surface area and their effect on drug loading capacity
title_full_unstemmed The role interplay between mesoporous silica pore volume and surface area and their effect on drug loading capacity
title_short The role interplay between mesoporous silica pore volume and surface area and their effect on drug loading capacity
title_sort role interplay between mesoporous silica pore volume and surface area and their effect on drug loading capacity
url http://www.sciencedirect.com/science/article/pii/S2590156719300222
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